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LY 367385

mGlu1a receptor antagonist CAS# 198419-91-9

LY 367385

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Chemical structure

LY 367385

3D structure

Chemical Properties of LY 367385

Cas No. 198419-91-9 SDF Download SDF
PubChem ID 5311261 Appearance Powder
Formula C10H11NO4 M.Wt 209.2
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in 1.1eq. NaOH
Chemical Name 4-[(S)-amino(carboxy)methyl]-3-methylbenzoic acid
SMILES CC1=C(C=CC(=C1)C(=O)O)C(C(=O)O)N
Standard InChIKey SGIKDIUCJAUSRD-QMMMGPOBSA-N
Standard InChI InChI=1S/C10H11NO4/c1-5-4-6(9(12)13)2-3-7(5)8(11)10(14)15/h2-4,8H,11H2,1H3,(H,12,13)(H,14,15)/t8-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of LY 367385

DescriptionA selective mGlu1a receptor antagonist, with an IC50 value of 8.8 μM for blockade of quisqualate-induced phosphoinositide hydrolysis vs. > 100 μM for mGlu5a, and negligible action on group II and III receptors. Also available as part of the Group I mGlu Receptor.

LY 367385 Dilution Calculator

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Preparing Stock Solutions of LY 367385

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.7801 mL 23.9006 mL 47.8011 mL 95.6023 mL 119.5029 mL
5 mM 0.956 mL 4.7801 mL 9.5602 mL 19.1205 mL 23.9006 mL
10 mM 0.478 mL 2.3901 mL 4.7801 mL 9.5602 mL 11.9503 mL
50 mM 0.0956 mL 0.478 mL 0.956 mL 1.912 mL 2.3901 mL
100 mM 0.0478 mL 0.239 mL 0.478 mL 0.956 mL 1.195 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on LY 367385

IC50: 8.8 μM

LY 367385 is a selective mGlu1a receptor antagonist for blockade of quisqualate-induced phosphoinositide hydrolysis.

The mGlu family of G-protein-linked glutamate receptors currently comprises eight members by 3,5-dihydroxyphenylglycine can activate specifically Group I mGlu receptors, which have been found to regulate multiple effects in the vertebrate brain.

In vitro: Compared with the activity of LY367385, the novel compound LY367366 antagonizes both mGlu1a and -5 receptors at low micromolar concentrations, but also recruits other subtypes at higher concentrations. LY367366 possessing neuroprotective ability was in general less efficacious than LY357385. This fact suggested that inhibitors of mGlu1 receptors is a potential agent to confer significant neuroprotection [1].

In vivo: LY 367385 and AIDA have been administered intracerebroventricularly (i.c.v.) to lethargic mice and DBAr2 mice, and focally into the inferior colliculus of GEPR. In lethargic mice both compounds significantly decrease the incidence of spontaneous spike and wave discharges on the electroencephalogram, after the administration of LY 367385, 250 nmol, i.c.v. LY 367385, 50 nmol, inhibites spontaneous spike and wave discharges from 30 to 60 min. In DBAr2 mice both compounds produce a rapid, transient suppression of sound-induced clonic seizures. In genetically epilepsy prone rats, both compounds decreases sound-induced clonic seizures. The results suggestes that antagonists of mGlu1 receptors are potential anticonvulsant tools and that activation of mGlu1 receptors likely contributes to a variety of epilepticsyndromes [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1].  Bruno V, Battaglia G, Kingston A, O'Neill MJ, Catania MV, Di Grezia R, Nicoletti F. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 receptors. Neuropharmacology. 1999 Feb;38(2):199-207.
[2].  Chapman AG, Yip PK, Yap JS, Quinn LP, Tang E, Harris JR, Meldrum BS. Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24.

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References on LY 367385

Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid).[Pubmed:10096765]

Eur J Pharmacol. 1999 Feb 26;368(1):17-24.

We have studied the effects in three rodent models of generalised convulsive or absence epilepsy of two antagonists of group I metabotropic glutamate receptors that are selective for the mGlu1 receptor. LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid) have been administered intracerebroventricularly (i.c.v.) to DBA/2 mice and lethargic mice (lh/lh), and focally into the inferior colliculus of genetically epilepsy prone rats (GEPR). In DBA/2 mice both compounds produce a rapid, transient suppression of sound-induced clonic seizures (LY 367385: ED50 = 12 nmol, i.c.v., 5 min; AIDA: ED50 = 79 nmol, i.c.v., 15 min). In lethargic mice both compounds significantly reduce the incidence of spontaneous spike and wave discharges on the electroencephalogram, from <30 to >150 min after the administration of AIDA, 500 nmol, i.c.v., and from 30 to >150 min after the administration of LY 367385, 250 nmol, i.c.v. LY 367385, 50 nmol, suppresses spontaneous spike and wave discharges from 30 to 60 min. In genetically epilepsy prone rats both compounds reduce sound-induced clonic seizures. LY 367385, 160 nmol bilaterally, fully suppresses clonic seizures after 2-4 h. AIDA is fully effective 30 min after 100 nmol bilaterally. It is concluded that antagonists of mGlu1 receptors are potential anticonvulsant agents and that activation of mGlu1 receptors probably contributes to a variety of epileptic syndromes.

Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 receptors.[Pubmed:10218860]

Neuropharmacology. 1999 Feb;38(2):199-207.

(+)-2-Methyl-4-carboxyphenylglycine (LY367385), a potent and selective antagonist of mGlu1a metabotropic glutamate receptors, was neuroprotective in the following in vitro and in vivo models of excitotoxic death: (i) mixed cultures of murine cortical cells transiently exposed to N-methyl-D-aspartate (NMDA); (ii) rats monolaterally infused with NMDA into the caudate nucleus; and (iii) gerbils subjected to transient global ischemia. We have compared the activity of LY367385 with that of the novel compound (+/-)-alpha-thioxantylmethyl-4-carboxyphenylglycine (LY367366), which antagonizes both mGlu1a and -5 receptors at low micromolar concentrations, but also recruits other subtypes at higher concentrations. Although LY367366 was neuroprotective, it was in general less efficacious than LY357385, suggesting that inhibition of mGlu1 receptors is sufficient to confer significant neuroprotection. We conclude that endogenous activation of mGlu1a receptors (or perhaps other mGlu1 receptor splice variants) contributes to the development of neuronal degeneration of excitotoxic origin.

Reduction of sensory and metabotropic glutamate receptor responses in the thalamus by the novel metabotropic glutamate receptor-1-selective antagonist S-2-methyl-4-carboxy-phenylglycine.[Pubmed:9639261]

Neuroscience. 1998 Aug;85(3):655-8.

Previous work has shown that responses of thalamic neurons in vivo to the metabotropic glutamate receptor agonists 1S,3R-aminocyclopentane-1,3-dicarboxylate and S-3,5-dihydroxyphenylglycine can be reduced by a variety of phenylglycine antagonists. Responses of thalamic neurons to noxious thermal somatosensory stimuli were reduced in parallel by these antagonists, indicating that these responses are mediated by Group I metabotropic glutamate receptors (i.e. metabotropic glutamate receptor-1 and/or metabotropic glutamate receptor-5), which are known to be linked to phosphoinositol phosphate hydrolysis. The recent development of S-2-methyl-4-carboxyphenylglycine as an antagonist which is highly selective for metabotropic glutamate receptor-1 compared to metabotropic glutamate receptor-5 on human receptors expressed in AV-12 cells, now offers the possibility of discriminating between these two receptor subtypes in order to distinguish which is involved in thalamic responses. We have made recordings from single somatosensory neurons in the thalamus of the rat, and find that S-2-methyl-4-carboxy-phenylglycine is able to reduce responses of neurons to 1S,3R-aminocyclopentane-1,3-dicarboxylate, S-3,5-dihydroxyphenylglycine, and noxious stimuli without significant effect on responses to either N-methyl-D-aspartate or (+/-)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate. These results suggest that excitatory responses of thalamic neurons to 1S,3R-aminocyclopentane-1,3-dicarboxylate and S-3,5-dihydroxyphenylglycine may be mediated by metabotropic glutamate receptor-1. Furthermore, the reduction of nociceptive responses by S-2-methyl-4-carboxy-phenylglycine indicates that metabotropic glutamate receptor-1 is involved in thalamic nociceptive processing and that such antagonists may have analgesic properties.

Description

LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.

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